- Discovery and optimization of imidazo[1,2-a]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R).
Discovery and optimization of imidazo[1,2-a]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R).
Bioorganic & medicinal chemistry letters (2008-12-23)
Kyle A Emmitte, Brian J Wilson, Erich W Baum, Holly K Emerson, Kevin W Kuntz, Kristen E Nailor, James M Salovich, Stephon C Smith, Mui Cheung, Roseanne M Gerding, Kirk L Stevens, David E Uehling, Robert A Mook, Ganesh S Moorthy, Scott H Dickerson, Anne M Hassell, M Anthony Leesnitzer, Lisa M Shewchuk, Arthur Groy, Jason L Rowand, Kelly Anderson, Charity L Atkins, Jingsong Yang, Peter Sabbatini, Rakesh Kumar
PMID19101143
摘要
The optimization of imidazo[1,2-a]pyridine inhibitors as potent and selective inhibitors of IGF-1R is presented. Further optimization of oral exposure in mice is also discussed. Detailed selectivity, in vitro activity, and in vivo PK profiles of an optimized compound is also highlighted.
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